Department of Chemistry, University of South Florida, Tampa, FL 33620, USA.
Bioorg Med Chem. 2011 Nov 15;19(22):6608-14. doi: 10.1016/j.bmc.2011.06.004. Epub 2011 Jun 16.
Palmerolides D-G are new bioactive macrolides isolated from the Antarctic tunicate Synoicum adareanum and are related to the melanoma-selective cytotoxin palmerolide A. Most of these palmerolides are potent V-ATPase inhibitors and have sub-micromolar activity against melanoma. Though palmerolide A remains the most potent of this series of natural products against mammalian V-ATPase, recent data suggests that palmerolide D is the most potent against melanoma. A comparison of the bioactivity data obtained for these natural product palmerolides has provided insight into the substructures necessary to retain V-ATPase inhibition and cytotoxic activity.
Palmerolides D-G 是从南极被囊动物 Synoicum adareanum 中分离得到的新型生物活性大环内酯类化合物，与黑色素瘤选择性细胞毒素 palmerolide A 有关。这些 palmerolides 大多数是强效的 V-ATPase 抑制剂，对黑色素瘤具有亚微摩尔活性。尽管 palmerolide A 仍然是该系列天然产物中对哺乳动物 V-ATPase 最有效的一种，但最近的数据表明 palmerolide D 对黑色素瘤的活性最强。对这些天然产物 palmerolides 的生物活性数据进行比较，深入了解了保留 V-ATPase 抑制和细胞毒性活性所必需的亚结构。
